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AG 494

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Chemical Structure| 133550-35-3 同义名 : Tyrphostin AG 494
CAS号 : 133550-35-3
货号 : A299892
分子式 : C16H12N2O3
纯度 : 99%+
分子量 : 280.278
MDL号 : MFCD00209863
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(374.63 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • EGFR/ErbB1

    EGFR, IC50:1.2 μM
描述 Many of the tyrosine kinase enzymes which are early components of the growth signal transduction pathway in mammalian cells are encoded by proto-oncogenes, and their transformation or overexpression has been shown to occur in a large percentage of clinical cancers. The epidermal growth factor receptor (EGFR), one of the tyrosine kinase enzymes, has thus become important target for cancer therapy [1]. AG-494 is capable of selectively inhibiting the EGFR tyrosine kinase activity in vitro as compared to a variety of tyrosine kinases, including the closely related HER-2/Neu receptor in the cell-free kinase assay. AG-494 inhibits autophosphorylation of EGFR with IC50 value of 1.1 ± 0.24 μM. AG-494 inhibits 50% of TPA (phorbol ester)- and LPA (lysophosphatidic acid)-dependent [3H]thymidine uptake at ~5 μM, whereas EGF-dependent [3H]thymidine uptake is inhibited at ~10.5 μM. These results imply that AG-494 exerts its antimitogenic effect by inhibiting a signal transduction element downstream of the EGFR [2]. EGF potentiates BMP9-induced early and late osteogenic markers of mesenchymal stem cells (MSCs), which can be effectively inhibited by AG-494 [3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.57mL

0.71mL

0.36mL

17.84mL

3.57mL

1.78mL

35.68mL

7.14mL

3.57mL
参考文献

[1]Bridges AJ. Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor. J Med Chem. 1996 Jan 5;39(1):267-76. doi: 10.1021/jm9503613.

[2]Osherov N, Levitzki A. Tyrphostin AG 494 blocks Cdk2 activation. FEBS Lett. 1997 Jun 30;410(2-3):187-90. doi: 10.1016/s0014-5793(97)00580-2.

[3]Liu X. Cross-talk between EGF and BMP9 signalling pathways regulates the osteogenic differentiation of mesenchymal stem cells. J Cell Mol Med. 2013 Sep;17(9):1160-72. doi: 10.1111/jcmm.12097. Epub 2013 Jul 11.